Assay Detail
Binding
CHEMBL4031179
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Binding affinity to human cGAS (2 to 522 residues) expressed in Sf9 insect cells by surface plasmon resonance assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of PF-06928215 as a high affinity inhibitor of cGAS enabled by a novel fluorescence polarization assay.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 5.29 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096573 | — | — | 1 | 6.70 |
| CHEMBL4084664 | — | — | 1 | 5.57 |
| CHEMBL4062994 | — | — | 1 | 5.17 |
| CHEMBL4103560 | — | — | 1 | 4.90 |
| CHEMBL4085628 | — | — | 1 | 4.11 |
| CHEMBL4065757 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096573 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL4084664 | — | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL4062994 | — | Kd | = | 6700.0 | nM | 5.17 |
| CHEMBL4103560 | — | Kd | = | 12500.0 | nM | 4.90 |
| CHEMBL4085628 | — | Kd | = | 78000.0 | nM | 4.11 |
| CHEMBL4065757 | — | Kd | = | 171000.0 | nM | - |